BRAND NAMES
 MECHANISM OF ACTION
Felodipine, is a long-acting dihydropyridine calcium channel blocker. It inhibits the influx of extra cellular calcium across the peripheral vascular smooth muscle cell membranes by binding directly to inactive L-type calcium channels, stabilizing their inactive conformation.
The decrease in intracellular calcium inhibits the contractile processes of the systemic arteries smooth muscle cells, and thus, decreases total peripheral resistance and systemic blood pressure.
Following administration of Felodipine, a reduction in blood pressure generally occurs within two to five hours. During chronic administration, substantial blood pressure control lasts for approximately 24 hours.
- Treatment of mild to moderate hypertension
- Adults: The usual recommended initial dose is 5 mg once daily with a light meal (Felodipine should not be administered with a meal rich in carbohydrates or fat). Depending on the patient's response, the dosage should be adjusted accordingly. Dose adjustment, if necessary, should be done at intervals of not less than two weeks. The maintenance dosage range is 2.5 to 10 mg once daily.
- Elderly: A starting dose no higher than 2.5 mg once daily is recommended. A dosage of 10 mg daily should not be exceeded
- Patients with a known hypersensitivity to felodipine or to other dihydropyridines.
- In women of childbearing potential, in pregnancy, and during lactation. Fetal malformations and adverse effects on pregnancy have been reported in animals.
 WARNINGS AND PRECAUTIONS
- Felodipine may lead to reflex tachycardia which, particularly in patients with severe obstructive coronary artery disease, may precipitate angina pectoris
- The consumption of grapefruit juice prior to or during treatment with Felodipine should be avoided. (grapefruit juice is an inhibitor of CYP3A4 and can increase plasma levels and augment pharmacodynamic effects of dihydropyridine calcium channel blockers).
- Felodipine may increase the concentration of tacrolimus. When used together, the tacrolimus serum concentration should be followed and the tacrolimus dose may need to be adjusted.
- Felodipine is extensively metabolized in humans, primarily by CYP3A4
- CYP3A4 inhibitors : CYP3A4 inhibitors like Ketoconazole, Itraconazole, Nefazodone, erythromycin, Clarithromycin, Isoniazid, fluvoxamine, Fluoxetine, HIV protease inhibitors (e.g. ritonavir, indinavir, nelfinavir) and Grapefruit juice can potentiate the effect of Felodipine
- CYP3A4 inducers (e.g. carbamazepine, efavirenz, St John’s wort, nevirapine, phenobarbitol, phenytoin, primidone, rifabutin, rifampicin) are expected to decrease Felodipine concentrations
 PREGNANCY AND LACTATION
- Pregnancy Category C (US). Fetal malformations and adverse effects on pregnancy have been reported in animals.
- Nursing: Discontinue when administering Felodipine.
 SIDE EFFECTS
- Most common:
- Mild to moderate peripheral edema of non-cardiac origin (local arterial dilatation seems to be involved rather than fluid retention), was the most common adverse event. Frequency ranged from about 10 percent in patients under 50 years of age taking 5 mg daily to about 30 percent in those over 60 years of age taking 20 mg daily. This adverse effect generally occurs within 2-3 weeks of the initiation of treatment.
Other possible adverse reactions:
- Mild gingival enlargement has been reported. Good dental hygiene decreases is incidence and severity.
 RELATED LINKS
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|Angiotensin II receptor antagonist||Azilsartan (Edarbi) • Candesartan (Atacand) • Eprosartan (Teveten) • Irbesartan (Aprovel, Avapro, Karvea) • Losartan (Cozaar) • Olmesartan (Benicar, Olmetec) • Telmisartan (Micadis) • Valsartan (Diovan, Tareg)|
|Renin inhibitors||Aliskiren (Rasilez, Tekturna)|
|Alpha-1 blockers||Doxazosin (Cardura) • Prazosin (Minipress) • Terazosin (Hytrin)|
|Alpha-2 agonists (centrally acting)||Clonidine (Oral route) • Clonidine (Transdermal) (Catapresan) • Guanfacine (Tenex) • Methyldopa (Aldomet)|
|Calcium channel blockers||Dihydropyridines||Amlodipine (Norvasc) • Barnidipine (Vasexten) • Felodipine (Plendil) • Isradipine (Dynacirc) • Lacidipine (Lacipil, Motens) • Lercanidipine (Zanidip) • Manidipine • Nicardipine • Nifedipine (Adalat) • Nisoldipine • Nitrendipine|
|Benzothiazepine||Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)|
|Phenylalkylamine||Gallopamil • Verapamil (Calan)|
|Beta blockers||Beta1 selective (cardioselective)||Acebutolol (Sectral) • Atenolol (Tenormin) • Betaxolol (Kerlon) • Bisoprolol (Concor) • Celiprolol (Cordiax) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Nebivolol (Bystolic, Lobivon, Nebilox)|
|Nonselective (Beta1 and Beta2 blockers)||Oxprenolol (Trasitensin) • Propranolol (Inderal) • Timolol (Blocadren)|
|Nonselective (Beta1, Beta2 and Alpha1 blockers)||Carvedilol (Dilatrend) • Labetalol (Trandate)|
|Beta blocker with intrinsic sympathomimetic activity (ISA)||Acebutolol (Sectral) • Celiprolol (Cordiax)|
|Lipophilic Beta blockers||Propranolol (Inderal) • Metoprolol (Betaloc, Lopressor, Toprol-XL) • Oxprenolol (Trasitensin)|
|Diuretics||Carbonic anhydrase inhibitors||Acetazolamide (Diamox)|
|Loop diuretics||Bumetanide • Etacrynic acid • Furosemide (Lasix) • Piretanide • Torasemide (Demadex)|
|Thiazide diuretics||Chlorothiazide (Diuril) • Hydrochlorothiazide (Esidrex)|
|Thiazide-like diuretics||Chlortalidone (Hygroton) • Indapamide (Lozol, Lozide) • Metolazone|
|Potassium-sparing diuretics|| Epithelial sodium channel blockers: Amiloride (Midamor) • Triamterene (Dyrenium) |
Aldosterone receptor antagonists: Potassium canrenoate • Eplerenone (Inspra) • Spironolactone (Aldactone)
|Combination therapy||Amiloride/Hydrochlorothiazide (Moduretic) • Spironolactone/Hydrochlorothiazide (Aldactazide)|